CAS: 5571-36-8; (8S,13S,14S)-13-Methyl-1,2,6,7,8,12,13,14,15,16-Decahydrospiro[cyclopenta[a]Phenanthrene-3,2'-[1,3]Dioxolan]-17(4H)-One

相似化合物

5571-36-8 42982-49-0 141299-95-8

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CAS号6218-29-7 甲基双烯醇酮 | CAS号5173-46-6 甲基双烯双酮 | CAS号126784-99-4 醋酸乌利司他 | CAS号6218-29-7 甲基双烯醇酮 | CAS号159811-51-5 乌利司他 | CAS号84371-57-3 (5α,10α,17β)-5,...

(8S,13S,14S,17S)-13-Methyl-1,2,4,6,7,8,12,13,14,15,16,17-Dodecahydrospiro[cyclopenta[a]Phenanthrene-3,2'-[1,3]Dioxolan]-17-Ol置于四丙基高钌酸铵,N-甲基吗啉氧化物体系中,用 二氯甲烷 作为反应溶剂,化学反应 0.25H,以99.3%的收率获得产物3-缩酮
参考文献:雄激素受体的高亲和力氟取代配体的合成.通过正电子发射断层扫描显像前列腺癌的潜在药物.
标题:雄激素受体的高亲和力氟取代配体的合成.通过正电子发射断层扫描显像前列腺癌的潜在药物.
摘要:我们已经制备了九种在c-16或c-20处被氟取代的雄激素,以评估其潜力,并在用正电子发射放射性核素氟18标记时作为前列腺癌的正电子发射断层显像(pet)成像剂(t1 / 2 = 110分钟).这些化合物代表以下雄激素的成员:睾丸激素(t),5α-二氢睾丸激素(dht),7α-甲基-19-睾丸激素(mnt),米泊洛酮(mib)和甲泼莫隆(r1881).所有这些化合物都是通过适当的雄激素前体官能化制备的,并且开发了合成路线以允许在合成后期通过氟离子置换反应引入氟,这是在氟18标记的化合物中制备这些化合物所需的形成.我们还制备了四个雄激素,其中c-3羰基或17个β-羟基被氟取代.大多数氟取代的雄激素对雄激素受体(ar)表现出高亲和力,尽管氟取代将其亲和力降低了一小部分.氟取代c-3或c-17处的氧官能团的雄激素都没有对ar有实质性的亲和力.天然雄激素的衍生物(t和dht)以及mnt与其他类固醇激
DOI:10.1021/jm00089A024

专利信息

专利号:US-8110691-B2
优先权日:2006-06-14
标题 :Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process
发明人：DANCSI LAJOSNE; VISKY GYOERGY; TUBA ZOLTAN; CSOERGEI JANOS; MOLNAR CSABA; MAGYARI ENDRENE
权利人:DANCSI LAJOSNE; VISKY GYOERGY; TUBA ZOLTAN; CSOERGEI JANOS; MOLNAR CSABA; MAGYARI ENDRENE; RICHTER GEDEON NYRT
摘要:A new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.

专利号:US-9676814-B2
优先权日:2013-10-01
标题:Industrial process for the synthesis of ulipristal acetate and its 4′-acetyl analogue
发明人：Mahó Sándor; SÃ?NTA CSABA; Csörgei János; Horváth János; ARANYI ANTAL; BÉNI ZOLTÃ?N
权利人:RICHTER GEDEON NYRT
摘要:The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.

专利号:US-8183402-B2
优先权日:2007-06-27
标 题:Industrial method for the synthesis of 17-acetoxy-11β[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process
发明人：BODI JOZSEF; VISKY GYOERGY; SZELES JANOS; MAHO SANDOR; SANTA CSABA; CSOERGEI JANOS; TUBA ZOLTAN; TERDY LASZLO; MOLNAR CSABA; ARANYI ANTAL; HORVATH ZOLTAN; BALOGH GABOR
权利人:BODI JOZSEF; VISKY GYOERGY; SZELES JANOS; MAHO SANDOR; SANTA CSABA; CSOERGEI JANOS; TUBA ZOLTAN; TERDY LASZLO; MOLNAR CSABA; ARANYI ANTAL; HORVATH ZOLTAN; BALOGH GABOR; RICHTER GEDEON NYRT
摘要:The present invention relates to a process for the synthesis of the 17-acetoxy-11β-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I): n nfrom 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II):

专利号:US-8314145-B2
优先权日:2005-12-05
标题 :High purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one and process for the synthesis thereof
发明人：DANCSI LAJOSNE; MAHO SANDOR; ARANYI ANTAL; HORVATH JANOS
权利人:DANCSI LAJOSNE; MAHO SANDOR; ARANYI ANTAL; HORVATH JANOS; RICHTER GEDEON VEGYESZET
摘要:The invention relates to a new process for the synthesis of high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents. According to our invention the dienogest of formula (I) is synthesized the following way: i) 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V) is reacted with aluminum isopropylate in the presence of cyclohexanone in an inert organic solvent under heating; ii) the so obtained 3-methoxy-estra-2,5(10)-diene-17-one of formula (IV) is reacted with cyanomethyl lithium at a temperature between 0 and −30° C.; iii) the obtained 3-methoxy-17α-cyanomethyl-17β-hydroxy-estra-2,5(10)-diene of formula (III) is reacted with a strong organic acid in tetrahydrofuran solution; iv) the obtained 17α-cyanomethyl-17β-hydroxy-estr-5(10)-ene-3-one of formula (II) is reacted with 1-1.5 equivalent of pyridinium tribromide in pyridine solution at a temperature between 0 and 60° C., then the obtained crude dienogest of formula (I) is purified by recrystallization and preparative HPLC.

专利号:US-9683010-B2
优先权日:2014-02-17
标 题 :Process for the production of 21-methoxy-11-beta-phenyl-19-nor-pregna-4,9-diene-3,20-dione derivatives
发明人：Mahó Sándor; SÃ?NTA CSABA; Csörgei János; Szabó Gábor; SCHÄFER TAMÃ?S; BÉNI ZOLTÃ?N
权利人:RICHTER GEDEON NYRT
摘要:The present invention relates to a process for the synthesis of compounds of formula (I), n nwherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R′ is dimethylamino or 2-methyl-1,3-dioxan-2-yl group, as starting material and methoxymethyl lithium as reagent.

专利号:US-2009187032-A1
优先权日:2006-06-14
标 题 :INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 17alpha-ACETOXY-11beta-[4-(N,N-DIMETHYL-AMINO)-PHENYL]-19-NORPREGNA-4,9-DIENE-3,20-DIONE AND NEW INTERMEDIATES OF THE PROCESS